Resatorvid (TAK-242)

製品コードS7455 バッチS745501

印刷

化学情報

Synonyms

CLI-095

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₅H₁₇ClFNO₄S

分子量

361.82

CAS No.

243984-11-4

Solubility (25°C)*

体外

DMSO

72 mg/mL (198.99 mM)

Ethanol

72 mg/mL (198.99 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Resatorvid (TAK-242, CLI-095) は、Toll様受容体 (TLR) 4シグナル伝達の小分子特異的阻害剤であり、マクロファージにおけるLPS誘導性のNO、TNF-α、およびIL-6の産生をそれぞれ1.8 nM、1.9 nM、および1.3 nMのIC50でブロックします。Resatorvidは、TLR4下流シグナル伝達分子であるMyD88とTRIFの発現を下方制御します。Resatorvidはオートファジーを阻害します。
in vitro	Resatorvid (TAK-242) inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. It disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM.
in vivo	Resatorvid (TAK-242) protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg. Topical application of this compound can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, it displays potent photochemopreventive activity, significantly suppressing tumor area and multiplicity. Tumors harvested from resatorvid-treated mice display reduced activity of UV-associated signaling pathways and a corresponding increase in apoptosis compared to tumors from control animals. It also significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Primary human keratinocytes
	濃度	10 µM
	反応時間	6 h
	実験の流れ	Keratinocytes are treated with UVB +/− 10 µM resatorvid (TAK-242) (or vehicle) and harvested 6 hr later. This compound significantly inhibits UV-induced NF-κB luciferase signaling in keratinocytes.
動物実験	動物モデル	male ddY mice aged 4-5weeks
	投薬量	1 μl (at 0.001, 0.03, or 0.01 μg/μl)
	投与方法	intracerebroventricularly

参考

https://pubmed.ncbi.nlm.nih.gov/28976923/
https://pubmed.ncbi.nlm.nih.gov/29437671/
https://pubmed.ncbi.nlm.nih.gov/23193438/

https://www.ncbi.nlm.nih.gov/pubmed/?term=27859308
https://pubmed.ncbi.nlm.nih.gov/16279805/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Activation of chicken macrophages by isomalto/malto-polysaccharide (IMMP) is facilitated by toll-like receptor 4 (TLR4) [ Poult Sci, 2025, 104(11):105690]	PubMed: 40848484
GATA1 Transcriptionally Upregulates LMCD1, Promoting Ferroptosis in Sepsis-Associated Acute Kidney Injury Through the Hippo/YAP Pathway [ Kaohsiung J Med Sci, 2025, e70071.]	PubMed: 40650665

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。